Splitomicin
Based on 1 Customer Validation
Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD+-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM.
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- Pureza: 98.34%
- No. CAS: 5690-03-9
- Fòrmula: C13H10O2
- Peso molecular:198.22
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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Sir2p 60 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| S2 | IC50 |
>10000 nM
Compound: splitomicin
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Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells
Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells
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[PMID: 19317450] |
Splitomicin (10-333 μM; 24 hours) elicits antiproliferative effects in MCF-7 and H1299 cells in a dose-dependent manner in colony formation assay. Splitomicin (33 μM) fails to decrease the number of colonies, but Splitomicin (100 and 333 μM) effectively inhibits colony formation in MCF-7 and H1299 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human breast cancer MCF-7 and lung cancer H1299 cells
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Concentration:10, 33, 100, and 333 μM
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Incubation Time:24 hours
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Result:Inhibited colony formation in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice aged 12-14 weeks weighing on average 27 g[3]
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Dosage:80 mg/kg
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Administration:Intraperitoneal injection every 24 h for 5 days
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Result:Increased TF activity in mouse carotid artery as compared with the controls.
Chemical Information
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No. CAS 5690-03-9
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Appearance Solid
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Peso molecular 198.22
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Fòrmula C13H10O2
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Color White to light yellow
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SMILES
O=C1CCC2=C3C=CC=CC3=CC=C2O1
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Synonyms
Splitomycin
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (504.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (10.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (10.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bedalov A, et al. Identification of a small molecule inhibitor of Sir2p. Proc Natl Acad Sci U S A. 2001 Dec 18;98(26):15113-8. [Content Brief]
[2]. Ota H, et al. Sirt1 inhibitor, Sirtinol, induces senescence-like growth arrest with attenuated Ras-MAPK signaling in human cancer cells. Oncogene. 2006 Jan 12;25(2):176-85. [Content Brief]
[3]. Breitenstein A, et al. Sirt1 inhibition promotes in vivo arterial thrombosis and tissue factor expression in stimulated cells. Cardiovasc Res. 2011 Feb 1;89(2):464-72. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.0449 mL | 25.2245 mL | 50.4490 mL | 126.1225 mL |
| 5 mM | 1.0090 mL | 5.0449 mL | 10.0898 mL | 25.2245 mL | |
| 10 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | 12.6122 mL | |
| 15 mM | 0.3363 mL | 1.6816 mL | 3.3633 mL | 8.4082 mL | |
| 20 mM | 0.2522 mL | 1.2612 mL | 2.5224 mL | 6.3061 mL | |
| 25 mM | 0.2018 mL | 1.0090 mL | 2.0180 mL | 5.0449 mL | |
| 30 mM | 0.1682 mL | 0.8408 mL | 1.6816 mL | 4.2041 mL | |
| 40 mM | 0.1261 mL | 0.6306 mL | 1.2612 mL | 3.1531 mL | |
| 50 mM | 0.1009 mL | 0.5045 mL | 1.0090 mL | 2.5224 mL | |
| 60 mM | 0.0841 mL | 0.4204 mL | 0.8408 mL | 2.1020 mL | |
| 80 mM | 0.0631 mL | 0.3153 mL | 0.6306 mL | 1.5765 mL | |
| 100 mM | 0.0504 mL | 0.2522 mL | 0.5045 mL | 1.2612 mL |
Splitomicin Related Classifications
HY-100585 Related Classifications
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